Virus-based expression systems facilitate rapid target in vivo functionality validation and high-throughput screening [0.03%]
基于病毒的表达系统可促进快速体内功能验证及高通量筛选
Andrew L Darrow,Kelly A Conway,Anil H Vaidya et al.
Andrew L Darrow et al.
Target validation is one of rate-limiting steps in the modern drug discovery. The authors developed a strategy of combining adenovirus-mediated gene transfer for efficient target functionality validation, both in vivo and in vitro, with bac...
Ionworks HT: a new high-throughput electrophysiology measurement platform [0.03%]
Ionworks HT：一种新的高通量电生理测量平台
Kirk Schroeder,Brad Neagle,Derek J Trezise et al.
Kirk Schroeder et al.
To address the throughput restrictions of classical patch clamp electrophysiology, Essen Instruments has developed a plate-based electrophysiology measurement platform. The instrument is an integrated platform that consists of computer-cont...
Galpha(16/z) chimeras efficiently link a wide range of G protein-coupled receptors to calcium mobilization [0.03%]
Gα(16/12)嵌合体可有效使多种G蛋白偶联受体激活钙动员响应
Andrew M F Liu,Maurice K C Ho,Cecilia S S Wong et al.
Andrew M F Liu et al.
G protein-coupled receptors (GPCRs) represent a class of important therapeutic targets for drug discovery. The integration of GPCRs into contemporary high-throughput functional assays is critically dependent on the presence of appropriate G...
Fluorescence polarization competition assay: the range of resolvable inhibitor potency is limited by the affinity of the fluorescent ligand [0.03%]
荧光偏振竞争测定法：荧光配体亲和力限制了解析抑制剂活性的范围
Xinyi Huang
Xinyi Huang
For the development of fluorescence polarization (FP) competition assays, there is a widespread belief that tight-binding fluorescent ligands should be avoided to identify inhibitors of low or intermediate potency in the screening of small-...
Single-molecule detection technologies in miniaturized high-throughput screening: fluorescence intensity distribution analysis [0.03%]
单分子检测技术在微型高通量筛选中的应用：荧光强度分布分析
Ulrich Haupts,Martin Rüdiger,Stephen Ashman et al.
Ulrich Haupts et al.
Single-molecule detection technologies are becoming a powerful readout format to support ultra-high-throughput screening. These methods are based on the analysis of fluorescence intensity fluctuations detected from a small confocal volume e...
Peter Ramm,Yuriy Alexandrov,Andrzej Cholewinski et al.
Peter Ramm et al.
Outgrowth of neurites in culture is used for assessing neurotrophic activity. Neurite measurements have been performed very slowly using manual methods or more efficiently with interactive image analysis systems. In contrast, medium-through...
Barbara A Kozikowski,Thomas M Burt,Debra A Tirey et al.
Barbara A Kozikowski et al.
A diverse set of 320 compounds from the Procter & Gamble Pharmaceuticals organic compound repository was prepared as 20-mM DMSO solutions and stored at 4 degrees C under argon in pressurized canisters to simulate a low-humidity environment....
The effect of room-temperature storage on the stability of compounds in DMSO [0.03%]
室温保存对DMSO中化合物稳定性的影响
Barbara A Kozikowski,Thomas M Burt,Debra A Tirey et al.
Barbara A Kozikowski et al.
The stability of approximately 7200 compounds stored as 20-mM DMSO solutions under ambient conditions was monitored for 1 year. Compound integrity was measured by flow injection analysis using positive and negative electrospray ionization m...
A generic high-throughput screening assay for kinases: protein kinase a as an example [0.03%]
一种激酶的通用高通量筛选实验方法及作为示例的蛋白激酶A
Rommel Mallari,Elissa Swearingen,Wei Liu et al.
Rommel Mallari et al.
A generic high-throughput screening assay based on the scintillation proximity assay technology has been developed for protein kinases. In this assay, the biotinylated (33)P-peptide product is captured onto polylysine Ysi bead via avidin. T...
Development of a versatile platform for nuclear receptor screening using AlphaScreen [0.03%]
开发用于核受体筛选的AlphaScreen多功能平台
Nathalie Rouleau,Sophie Turcotte,Marie-Hélène Mondou et al.
Nathalie Rouleau et al.
The interaction between nuclear receptors (NRs) and their coactivators, a key step in transcription regulation, requires a short consensus sequence called the LXXLL motif found in the coactivators' structure. Using the AlphaScreen technolog...